Evidence map›Paper›PMID 29125744›Full record

ArticleJournal of medicinal chemistry2017

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors.

Tracy Bayliss, David A Robinson, Victoria C Smith, Stephen Brand, Stuart P McElroy, Leah S Torrie, Chido Mpamhanga, Suzanne Norval, Laste Stojanovski, Ruth Brenk and 4 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

11 citing papers in PubMed.

  1. Article
  2. Molecules (Basel, Switzerland) · 2025
    Review
  3. A Selection Protocol to Identify Therapeutics to Target NLRP3-Associated Sensory Hearing Loss.Otology & neurotology : official publication of the American Otological Society, American Neurotology Society [and] European Academy of Otology and Neurotology · 2024
    Article
  4. Review
  5. Review
  6. Microbiology spectrum · 2023
    Article
  7. Article
  8. Review
  9. Article
  10. Exploring NovelACS omega · 2019
    Article
  11. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

14 authors.

Tracy BaylissDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
David A RobinsonDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.ORCID 0000-0003-1979-5918
Victoria C SmithDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Stephen BrandDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Stuart P McElroyDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Leah S TorrieDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Chido MpamhangaDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Suzanne NorvalDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Laste StojanovskiDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Ruth BrenkDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Julie A FrearsonDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Kevin D ReadDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
Ian H GilbertDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.ORCID 0000-0002-5238-1314
Paul G WyattDrug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.ORCID 0000-0002-0397-245X

Funding

Wellcome Trust 203134Wellcome Trust 203134/Z/16/Z
6 · The paper itself

Abstract

N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trypanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stages 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a starting point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT.

Indexed as

AcyltransferasesAminopyridinesAnimalsBenzenesulfonamidesBrainCrystallography, X-RayDrug DesignEnzyme InhibitorsHumansMiceSulfonamidesTrypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, AfricanAcyltransferasesAminopyridinesBenzenesulfonamidesDDD 85646Enzyme Inhibitorsglycylpeptide N-tetradecanoyltransferaseSulfonamidesTrypanocidal Agents

Identifiers

PMID29125744
PMCPMC5734605

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.